Work is in progress to confirm preliminary observations that oral administration of beta-glycerophosphate (beta-GP) stimulates hepatic synthesis and secretion into bile of biliary phospholipids. This has the potential of increasing solubility of cholesterol in bile. Thus, it may undersaturate bile in patients with bile supersaturated with cholesterol. Therefore, it is considered to be a potential drug for dissolution and prevention of gallstones. Long-term toxicity studies in rodents and primates did not show evidence for harmful side effects and long term studies in five patients with cholesterol gallstones did not demonstrate any toxic effects. Having completed toxicity studies in primates, studies are now in progress to study the effect of beta-GP, quantitatively on biliary lipids in healthy volunteers. Furthermore, radioactive beta-GP compounds have now been synthesized for studying the metabolic pathways of beta-GP. Preliminary studies in patients with cholilithiasis and hypercholesterolemia have shown a blood cholesterol lowering effect in four out of five patients. Furthermore studies are now in progress to validate these observations in patients with hypercholesterolemia.